Department of Chemical Engineering, Federal University of Ceará, Fortaleza, CE, Brazil.
Laboratory of Chemistry of Natural Products, Center for Science and Technology, State University of Ceará, Fortaleza, CE, Brazil.
Int J Biol Macromol. 2021 Jan 15;167:1361-1370. doi: 10.1016/j.ijbiomac.2020.11.090. Epub 2020 Nov 17.
Essential oils (EOs) are bioactive compounds with therapeutic potential for use as alternatives or as support to conventional treatments. However, EOs present limitations, such as sensibility to environmental factors, which can be overcome through microencapsulation. The objective of this study was to produce, by spray drying, chitosan microparticles (CMs) loaded with EO of Lemongrass (Cymbopogon flexuosus), Geranium (Pelargonium x ssp) and Copaiba (Copaifera officinalis). Physicochemical and biological characterization of these microparticles showed that CMs presented spherical morphology, had an average size range of 2-3 μm with positive zeta potential (ZP) values, and enhanced thermal stability, compared to free EO. The encapsulation efficiency (EE) ranged from 4.8-58.6%, depending on the oil's properties. In vitro EO release from CMs was determined at different pHs, with 94% release observed in acid media. All microparticles were non-hemolytic at concentrations of up to 0.1 mg·mL. EOs and CMs presented acetylcholinesterase (AChE) inhibition activity (IC 50 ranged from 11.92 to 28.18 μg·mL). Geranium and Copaiba EOs presented higher toxicity against Artemia salina, and greater inhibition of acetylcholinesterase, indicating potential bioactivity for Alzheimer's disease (AD). Our findings demonstrate that CM systems may show promise for the controlled release of these EOs.
精油(EOs)是具有治疗潜力的生物活性化合物,可作为替代传统治疗方法或作为传统治疗方法的辅助手段。然而,EOs 存在一些局限性,例如对环境因素敏感,这些局限性可以通过微胶囊化来克服。本研究的目的是通过喷雾干燥法制备负载柠檬草(Cymbopogon flexuosus)、天竺葵(Pelargonium x ssp)和巴西可可巴(Copaifera officinalis)精油的壳聚糖微球(CMs)。这些微球的物理化学和生物学特性表明,CMs 呈现出球形形态,平均粒径范围为 2-3μm,具有正的 Zeta 电位(ZP)值,与游离 EO 相比,热稳定性得到增强。包封效率(EE)范围为 4.8-58.6%,具体取决于油的性质。在不同的 pH 值下测定了 CMs 中 EO 的体外释放情况,在酸性介质中观察到 94%的释放。所有微球在高达 0.1mg·mL 的浓度下均无溶血作用。EOs 和 CMs 对乙酰胆碱酯酶(AChE)具有抑制活性(IC 50 范围为 11.92 至 28.18μg·mL)。天竺葵和巴西可可巴 EOs 对卤虫的毒性更高,对乙酰胆碱酯酶的抑制作用更强,表明其对阿尔茨海默病(AD)具有潜在的生物活性。我们的研究结果表明,CM 系统可能在这些 EOs 的控制释放方面具有潜力。